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十取代芦丁硫酸钠(RDS)作为一种补体免疫抑制剂对恒温动物和人类免疫缺陷病毒(HIV)具有很高活性。本文采用离子对固相萃取技术(IP-SPE)从大鼠血浆、尿液、胆汁和蛋白溶液中分离提取十取代芦丁硫酸钠,并考察了十取代芦丁硫酸钠静脉注射后的药动学参数、排泄(包括尿液和胆汁)和蛋白结合情况。大鼠尾静脉注射给药3个剂量(5、20和100mg·kg?1)后,药-时曲线数据用药动学软件进行拟合,符合静脉注射二室模型,平均消除半衰期t1/2β为3.432±0.1852h,并且给药剂量与AUC具有良好的线性关系,药动学参数与给药剂量无关,提示十取代芦丁硫酸钠在大鼠体内的处置情况属于线性动力学。大鼠尾静脉注射十取代芦丁硫酸钠(20mg·kg?1)后,尿液和胆汁的累积排泄率分别为86.0%±6.1%和0.3181%±0.2087%。十取代芦丁硫酸钠与SD大鼠、Beagle犬和人血浆蛋白结合率为80%～90%,与HSA为85.7%±1.3%,而与人α1-AGP则为14.0%±3.2%,两者之间有极显著性差异(P<0.001)。
Sodium decyl substituted rutin sulfate (RDS) as a complement immunosuppressive agent is highly active against warm-blooded animals and human immunodeficiency virus (HIV). In this paper, ion-pair solid-phase extraction technology (IP-SPE) was used to separate and extract ten-substituted sodium rutin sulfate from plasma, urine, bile and protein solution of rats. Learning parameters, excretion (including urine and bile) and protein binding. After 3 doses (5, 20 and 100 mg · kg -1) were injected into the tail vein of rats, the drug-time curve data were fitted by pharmacokinetics software and fitted with intravenous injection of two-compartment model. The mean half-life t1 / 2β was 3.432 ± 0.1852h, and the dose and the AUC has a good linear relationship between the pharmacokinetic parameters and dose has nothing to do, suggesting that the ten substituted sodium rutin sulfate treatment in rats are linear kinetics. The cumulative excretion rates of urine and bile were 86.0% ± 6.1% and 0.3181% ± 0.2087%, respectively, after the rats were injected intravenously with ten substituted sodium rutin sulfate (20 mg · kg -1). Substitution rate of sodium rutin sulfate with SD rats, Beagle dogs and human plasma protein was 80% -90%, with HSA 85.7% ± 1.3%, while with human α1-AGP 14.0% ± 3.2% There was a significant difference between the two groups (P <0.001).